2019
DOI: 10.1021/acs.molpharmaceut.9b00670
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Epidermal Growth Factor Receptor-Targeted Delivery of a Singlet-Oxygen Sensitizer with Thermal Controlled Release for Efficient Anticancer Therapy

Abstract: Photodynamic therapy (PDT) utilizing lightinduced singlet oxygen has achieved attractive results in anticancer fields; however, its development is hindered by limited light penetration depth, skin phototoxicity, tumor hypoxia, and PDT-induced hypoxia. Inspired by our previous research work and the limitations of PDT, we introduce a smallmolecule-targeted drug erlotinib into the singlet-oxygen chemical source endoperoxide to achieve an EGFR-targeted PDT-mimetic sensitizer (Y3-1) for anticancer therapy. We demon… Show more

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Cited by 14 publications
(12 citation statements)
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“…The rate constant of 1 O 2 generation was calculated to be 0.03971 based on a reported method using 1,3-diphenylisobenzofuran (DPBF) as the reference (Figure S10). As seen in Figure F and S11, the efficiency of 1 O 2 generation was greatly enhanced in Hb-contained groups. These results demonstrated that Hb had a major contribution to the 1 O 2 generation.…”
Section: Results and Discussionmentioning
confidence: 76%
“…The rate constant of 1 O 2 generation was calculated to be 0.03971 based on a reported method using 1,3-diphenylisobenzofuran (DPBF) as the reference (Figure S10). As seen in Figure F and S11, the efficiency of 1 O 2 generation was greatly enhanced in Hb-contained groups. These results demonstrated that Hb had a major contribution to the 1 O 2 generation.…”
Section: Results and Discussionmentioning
confidence: 76%
“…[23] Finally,t his methodology was also applied in the derivatization of Erlotinib, whichisoften used for molecular targeted therapy, to yield 5k.A so bserved in almosta ll cases, the PcAACr eaction showede xcellent selectivity,c onversions,a nd yields,w hich represents an important finding fort he preparation of 1,4-substituted 1,2,3-triazolesw ithout the use of copper. [24] In addition, to illustrate the practicability of the reaction protocol, the PcAACr eaction could be scaled up to 1g by using 0.5 mol of the each reactant, giving as atisfactory yield of 88 % [c] [(piq) 2 Ir(acac)] DCM 6/RT,a ir,w hite LED NR 19 [d] [(piq) 2 Ir(acac)] DCM 6/RT,a ir,w hite LED NR catalystr etains its catalytic activity during continuous recycling experiments (four cycles) with considerable selectivity and efficiency. The development of solars ynthesis for organic photochemistry is ah ighly significant advance [25] because sunlight is effectively an inexhaustible energy source.…”
Section: Resultsmentioning
confidence: 99%
“…These factors, together with other pro-angiogenic factors, they promote the growth of excessive tumor vasculature in tumors. Erlotinib (ERL), a tyrosine inhibitor that specifically targets tumor cells, , has been shown to normalize tumor vasculature. − …”
Section: Introductionmentioning
confidence: 99%
“…These factors, together with other pro-angiogenic factors, they promote the growth of excessive tumor vasculature in tumors. Erlotinib (ERL), a tyrosine inhibitor that specifically targets tumor cells, 11,12 has been shown to normalize tumor vasculature. 13−16 Normalization of blood vessels can repair the structure and function of tumor vasculature by correcting angiogenesis signals.…”
Section: Introductionmentioning
confidence: 99%